(-)-Enitociclib ((R)-Enitociclib) is an enantiomer of Enitociclib with an optical rotation of (-). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC + lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib and Lenalidomide, and can be used in the research of hematological malignancies [1] [2].
In Vitro, CDK9 drives transcriptional elongation of RNA polymerase II to sustain the continuous expression of key oncogenic proteins such as MCL-1 and MYC, thereby promoting tumor cell proliferation and survival; inhibition of CDK9 rapidly induces the degradation of these proteins, leading to tumor cell killing, and holds research value in both hematologic malignancies and solid tumors.
References:
[1]. Frigault MM, et al. Enitociclib, a Selective CDK9 Inhibitor, Induces Complete Regression of MYC+ Lymphoma by Downregulation of RNA Polymerase II Mediated Transcription. Cancer Res Commun. 2023 Nov 9;3(11):2268-2279.
[2]. Tran S, et al. Enitociclib, a selective CDK9 inhibitor: in vitro and in vivo preclinical studies in multiple myeloma[J]. Blood Neoplasia, 2025, 2(1): 100050.
In Vitro, CDK9 drives transcriptional elongation of RNA polymerase II to sustain the continuous expression of key oncogenic proteins such as MCL-1 and MYC, thereby promoting tumor cell proliferation and survival; inhibition of CDK9 rapidly induces the degradation of these proteins, leading to tumor cell killing, and holds research value in both hematologic malignancies and solid tumors.
References:
[1]. Frigault MM, et al. Enitociclib, a Selective CDK9 Inhibitor, Induces Complete Regression of MYC+ Lymphoma by Downregulation of RNA Polymerase II Mediated Transcription. Cancer Res Commun. 2023 Nov 9;3(11):2268-2279.
[2]. Tran S, et al. Enitociclib, a selective CDK9 inhibitor: in vitro and in vivo preclinical studies in multiple myeloma[J]. Blood Neoplasia, 2025, 2(1): 100050.